What neurotransmitter is found in beta cells in pancreas and is released along with insulin?

serotonin

What type of impairment has a more detrimental effect on insulin levels-- kidney or liver?

kidney

what is the most commonly used clinical marker utilized to screen for diabetes?

Hemoglobin A1C

This is a yellow fluorescent AGE that is formed when arginine groups in proteins react with methylglyoxal that has built up inside cells during hyperglycemia?

Arg-pyrimidine

____ insulin differs from human by substitution of 1 different AA?

porcine

_____ insulin differs from human by substitution of 2 different AAs?

bovine

What is the normal range of glucose when fasted?

70-130 mg/dl

What drugs can cause hypoglycemia?

ethanol

beta adrenergic receptor antagonists

salicylates

What drugs can cause hyperglycemia?

epinephrine

glucocorts

oral contraceptives

phenytoin

clonidine

calcium channel blockers

diuretics

These drugs stimulate the release of insulin from beta cells by binding to and blocking an ATP-ase sensitive K+ channel, which causes depolarization and an increase in intracellular calcium which leads to release of insulin?

sulfonylureas

These drugs may also decrease the hepatic clearance of insulin?

sulfonylureas

Are first gen or second gen sulfonylureas 100 times more potent?

second gen

The dosage must be individualized for these oral hypoglycemic agents?

sulfonylureas

Name the four first gen sulfonylureas.

Tolazamide (Tolinase)

Chlorpropamide (Diabinese)

Tolbutamide (Orinase)

Acetohexamide (Dymelor)

Which first gen sulfonylurea has no active metabolites?

Tolbutamide

Which first gen sulfonylurea has the longest serum half life of 36 hours and is therefore the longest acting?

Chlorpropamide

List first gen sulfonylureas in order of increasing half lives starting with the shortest half life.

Tolbutamide

Acetohexamide (6-8)

Tolazamide (7)

Chlorpropamide

Name the two second gen sulfonylureas.

Glipizide

Glyburide

Which second gen sulfonylurea has no active metabolites?

glipizide

Name the third gen sulfonylurea.

glimepiride (Amaryl)

What is the half life of glimepiride?

9 hours

What are the addtl MOAs of glimepiride?

appears to translocate GLUT4 to the cell surface -- insulin like activity

may bind to a different protein than the usual sulfonylurea receptor on the beta cell

What is the indication for sulfonylureas?

control glucose in Type 2 when diet and exercise do not work

What is the pKa of sulfonylureas?

5

What is the most common side effect of the sulfonylureas?

hypoglycemia

lots of DIs

What is the indication for the thiazolidinediones?

for Type 2

alone or in combo with sulfonylurea or insulin

These drugs could cause hepatic failure?

thiazolidinediones

Monitor transaminase levels before and after starting therapy with these drugs?

thiazolidinediones

Name the two thiazolidinediones.

rosiglitazone (Avandia)

pioglitazone (Actos)

Which thiazolid is metabolized by 2C8 (and to a lesser extent by 2C9)?

rosiglitazone

Which thiazolid is metabolized by 3A4?

pioglitazone

These drugs increase the activity of nuclear receptor PPAR gamma that regulates genes responsible for the control of glucose and insulin metabolism in adipose, liver and skeletal muscle tissues, which increases tissue sensitivity?

thiazolids

These drugs need to be taken with additional BC other than OCs?

thiazolids (mainly pioglitazone)

These drugs are contraindicated in patients at risk for heart failure?

thiazolids

What is a common side effect when taking thiazolids?

edema

This drug is a non-sulfonylurea analog of glyburide?

repaglinide (Prandin)

What enzyme metabolizes Prandin?

3A4

this drug is for Type 2 w/ diet and exercise and can be used in combo with a thiazolid?

prandin

This drug stimulates the release of insulin in beta cells by binding to and blocking an ATPase sensitive K+ channel, which causes depolarization and an increase in intracellular calcium, which leads to release of insulin? May also decrease hepatic clearance of insulin and is a miscellaneous non-sulf?

Prandin

This drug can decrease vit B12 and folate absorption?

metformin

This drug's half life is only 1.3-4.5 hours?

metformin

This drug has no protein binding and no metabolism with rapid renal excretion?

metformin

You should STOP taking this drug if you have an MI or septicemia?

metformin

Metformin

Glucophage

Nateglinide

Starlix

T/F: metformin causes insulin release in the pancreas.

false

This drug is for Type 2 with diet and exercise and can be used in combo with a sulfonylurea?

metformin

Acarbose

Precose

Repaglinide

Prandin

Pioglitazone

Actos

Rosiglitazone

Avandia

Glimepiride

Amaryl

Glyburide

DiaBeta

Micronase

Glynase PresTab

Glipizide

Glucotrol

Tolazamide

Tolinase

Tolbutamide

Orinase

Chlorpropamide

Diabinese

Acetohexamide

Dymelor

This drug decreases hepatic gluconeogenesis and intestinal glucose absorption, increases peripheral tissue insulin sensititivity, and does NOT cause insulin release in the pancreas?

metformin

This drug is a D-phenylglycine and is unrelated to the sulfonylureas?

Starlix

Miglitol

Glyset

What enzymes metabolize Starlix?

2C9 = 70%

3A4 = 30%

This drug is highly selective with low affinity for heart and skeletal muscle potassium channels and has 98% albumin binding?